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Assay Detail

CHEMBL4196283

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiproliferative activity human HT-29 cells after 48 hrs by propidium iodide staining-based fluorescence assay
15
Total Activities
15
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type HT-29
Confidence 1 — Organism
Curated By Intermediate

Target

HT-29 (CHEMBL384)
Type CELL-LINE
Organism Homo sapiens

Publication

Design, synthesis, mechanistic and histopathological studies of small-molecules of novel indole-2-carboxamides and pyrazino[1,2-a]indol-1(2H)-ones as potential anticancer agents effecting the reactive oxygen species production.
Youssif BGM, Abdelrahman MH, Abdelazeem AH, Abdelgawad MA, Ibrahim HM, Salem OIA, Mohamed MFA, Treambleau L, Bukhari SNA.
Eur J Med Chem (2018) 146 : 260 -273
PubMed 29407956 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 5.47 7.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL553 ERLOTINIB 4.0 1 7.70
CHEMBL4208224 1 6.22
CHEMBL4208745 1 6.05
CHEMBL4213146 1 6.05
CHEMBL4207316 1 5.72
CHEMBL4214496 1 5.62
CHEMBL4209588 1 5.54
CHEMBL4203868 1 5.32
CHEMBL4213991 1 5.19
CHEMBL4216082 1 5.11
CHEMBL4215183 1 4.91
CHEMBL4204413 1 4.86
CHEMBL4218912 1 4.77
CHEMBL4212603 1 4.56
CHEMBL4205206 1 4.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL553 ERLOTINIB IC50 = 20.0 nM 7.70
CHEMBL4208224 IC50 = 600.0 nM 6.22
CHEMBL4208745 IC50 = 900.0 nM 6.05
CHEMBL4213146 IC50 = 900.0 nM 6.05
CHEMBL4207316 IC50 = 1900.0 nM 5.72
CHEMBL4214496 IC50 = 2400.0 nM 5.62
CHEMBL4209588 IC50 = 2900.0 nM 5.54
CHEMBL4203868 IC50 = 4800.0 nM 5.32
CHEMBL4213991 IC50 = 6500.0 nM 5.19
CHEMBL4216082 IC50 = 7700.0 nM 5.11
CHEMBL4215183 IC50 = 12200.0 nM 4.91
CHEMBL4204413 IC50 = 13800.0 nM 4.86
CHEMBL4218912 IC50 = 16900.0 nM 4.77
CHEMBL4212603 IC50 = 27800.0 nM 4.56
CHEMBL4205206 IC50 = 34700.0 nM 4.46